EP1669350A4 - Novel piperidine derivative - Google Patents

Novel piperidine derivative

Info

Publication number
EP1669350A4
EP1669350A4 EP04787951A EP04787951A EP1669350A4 EP 1669350 A4 EP1669350 A4 EP 1669350A4 EP 04787951 A EP04787951 A EP 04787951A EP 04787951 A EP04787951 A EP 04787951A EP 1669350 A4 EP1669350 A4 EP 1669350A4
Authority
EP
European Patent Office
Prior art keywords
disorder
sleep
insomnia
system diseases
histamine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP04787951A
Other languages
German (de)
French (fr)
Other versions
EP1669350A1 (en
EP1669350B1 (en
Inventor
N Ohtake
Sayaka Mizutani
Ryo Yoshimoto
Shigeru Tokita
Akio Kanatani
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
MSD KK
Original Assignee
Banyu Phamaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Banyu Phamaceutical Co Ltd filed Critical Banyu Phamaceutical Co Ltd
Publication of EP1669350A1 publication Critical patent/EP1669350A1/en
Publication of EP1669350A4 publication Critical patent/EP1669350A4/en
Application granted granted Critical
Publication of EP1669350B1 publication Critical patent/EP1669350B1/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver; circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypetsomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic imsomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X 1 and X 2 independently represent a nitrogen atom or CH; Y represents a specific goup; X 3 represents O s -(CH 2 ) m ; R 1 and R 2 independently represent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substitued with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
EP04787951A 2003-09-22 2004-09-21 Piperidine derivatives Expired - Lifetime EP1669350B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2003330758 2003-09-22
PCT/JP2004/013768 WO2005028438A1 (en) 2003-09-22 2004-09-21 Novel piperidine derivative

Publications (3)

Publication Number Publication Date
EP1669350A1 EP1669350A1 (en) 2006-06-14
EP1669350A4 true EP1669350A4 (en) 2009-05-06
EP1669350B1 EP1669350B1 (en) 2012-02-29

Family

ID=34373028

Family Applications (1)

Application Number Title Priority Date Filing Date
EP04787951A Expired - Lifetime EP1669350B1 (en) 2003-09-22 2004-09-21 Piperidine derivatives

Country Status (8)

Country Link
US (2) US7547693B2 (en)
EP (1) EP1669350B1 (en)
JP (1) JP4765627B2 (en)
CN (1) CN1902177A (en)
AT (1) ATE547404T1 (en)
AU (1) AU2004274309B2 (en)
CA (1) CA2551037A1 (en)
WO (1) WO2005028438A1 (en)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030236259A1 (en) * 2002-02-05 2003-12-25 Rolf Hohlweg Novel aryl- and heteroarylpiperazines
AU2004274309B2 (en) * 2003-09-22 2010-04-08 Msd K.K. Novel piperidine derivative
SE0401971D0 (en) * 2004-08-02 2004-08-02 Astrazeneca Ab Piperidne derivatives
EP1707203A1 (en) * 2005-04-01 2006-10-04 Bioprojet Treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia with non-imidazole alkylamines histamine H3- receptor ligands
EP1892241B1 (en) * 2005-05-30 2016-03-30 Msd K.K. Novel piperidine derivative
RU2442775C2 (en) * 2005-07-04 2012-02-20 Хай Пойнт Фармасьютикалс, ЛЛС Histamine nz-receptor antagonists
EP2233470B1 (en) 2005-07-04 2011-12-07 High Point Pharmaceuticals, LLC Histamine H3 receptor antagonists
US8158673B2 (en) * 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
TWI385169B (en) * 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd Heterocyclic substituted pyridine derivatives and antifungal agent containing same
JP4371164B2 (en) * 2005-11-10 2009-11-25 萬有製薬株式会社 Aza-substituted spiro derivatives
JP2009532418A (en) 2006-04-07 2009-09-10 ハイ ポイント ファーマシューティカルズ,リミティド ライアビリティ カンパニー 11β-Hydroxysteroid dehydrogenase type 1 active compound
SG163547A1 (en) * 2006-05-29 2010-08-30 High Point Pharmaceuticals Llc 3- (1, 3-benz0di0x0l-5-yl) -6- (4-cyclopropylpiperazin-1-yl) -pyridazine, its salts and solvates and its use as histamine h3 receptor antagonist
CA2657078A1 (en) 2006-07-13 2008-01-17 High Point Pharmaceuticals, Llc 11beta-hydroxysteroid dehydrogenase type 1 active compounds
EP1878721A1 (en) * 2006-07-13 2008-01-16 Novo Nordisk A/S 4-Piperidylbenzamides as 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
US8324240B2 (en) 2007-03-20 2012-12-04 Curis, Inc. Fused amino pyridine as HSP90 inhibitors
JP5520816B2 (en) 2007-05-04 2014-06-11 アストラゼネカ・アクチエボラーグ Process for the synthesis of alkylphosphinic acids starting with amines and amine oxides
ATE508110T1 (en) * 2007-06-05 2011-05-15 Nsab Af Neurosearch Sweden Ab NEW DISUBSTITUTED PHENYLPYRROLIDINES AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION
CA2690091A1 (en) 2007-06-05 2008-12-11 Nsab, Filial Af Neurosearch Sweden Ab, Sverige New disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission
EP2014656A3 (en) * 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC New heteocyclic h3 antagonists
CA2702265C (en) * 2007-10-11 2014-12-02 Smithkline Beecham Corporation Novel seh inhibitors and their use
EP2240025A4 (en) * 2008-01-30 2012-03-28 Glaxosmithkline Llc NOVEL sEH INHIBITORS AND THEIR USE
US20100324076A1 (en) * 2008-01-30 2010-12-23 Joseph Paul Marino Novel sEH Inhibitors and their Use
WO2009097476A1 (en) * 2008-01-30 2009-08-06 Smithkline Beecham Corporation NOVEL sEH INHIBITORS AND THEIR USE
AR074466A1 (en) 2008-12-05 2011-01-19 Sanofi Aventis PIPERIDINE ESPIRO PIRROLIDINONA AND PIPERIDINONA REPLACED AND ITS THERAPEUTIC USE IN DISEASES MEDIATED BY THE MODULATION OF H3 RECEPTORS.
AR074467A1 (en) 2008-12-05 2011-01-19 Sanofi Aventis TETRAHIDROPIRAN ESPIRO PIRROLIDINONES AND REPLACED PIPERIDINONES, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN AND USE THEMSELVES IN THE TREATMENT AND / OR PREVENTION OF CNS DISEASES, SUCH AS ALZHEIMER AND PARKINSON, BETWEEN OZ.
EP2387316A4 (en) 2009-01-16 2012-06-13 Curis Inc Fused amino pyridines for the treatment of brain tumors
WO2011143145A1 (en) 2010-05-11 2011-11-17 Sanofi Substituted n-alkyl and n-acyl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof
EP2569304A1 (en) 2010-05-11 2013-03-20 Sanofi Substituted n-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
EP2569294B1 (en) 2010-05-11 2015-03-11 Sanofi Substituted n-heteroaryl bipyrrolidine carboxamides, preparation and therapeutic use thereof
EP2569297A1 (en) 2010-05-11 2013-03-20 Sanofi Substituted n-heterocycloalkyl bipyrrolidinylphenyl amide derivatives, preparation and therapeutic use thereof
JP5968307B2 (en) 2010-05-11 2016-08-10 サノフイ Substituted phenylcycloalkylpyrrolidine (piperidine) spirolactams and amides, their preparation and therapeutic use
JP5784110B2 (en) * 2010-05-11 2015-09-24 サノフイ Substituted N-heteroaryltetrahydro-isoquinoline derivatives, their preparation and therapeutic use
CN103201267B (en) 2010-07-29 2016-08-17 里格尔药品股份有限公司 AMPK-activity heterocyclic compound and its using method
WO2013130935A1 (en) * 2012-03-02 2013-09-06 Genentech, Inc. Amido-benzyl sulfoxide derivatives
WO2013130943A1 (en) * 2012-03-02 2013-09-06 Genentech, Inc. Alkyl-and di-substituted amido-benzyl sulfonamide derivatives
DK2884978T3 (en) * 2012-08-16 2019-09-30 Scripps Research Inst New Kappa opioid ligand
WO2017083219A1 (en) * 2015-11-12 2017-05-18 Merck Sharp & Dohme Corp. Bispiperidinyl derivatives as liver x receptor beta agonists, compositions, and their use
WO2018068296A1 (en) 2016-10-14 2018-04-19 Merck Sharp & Dohme Corp. PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
WO2018068297A1 (en) * 2016-10-14 2018-04-19 Merck Sharp & Dohme Corp. N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
TW202216705A (en) 2020-07-17 2022-05-01 日商衛材R&D企管股份有限公司 Substituted piperidine compound and application thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3951982A (en) * 1974-11-21 1976-04-20 Parke, Davis & Company Trialkylsilyl esters of 6(substituted amino)phenyl-1,-dihydro-2-oxonicotinic acid, methods for their production and conversion to the corresponding acid chlorides
WO2000026192A1 (en) * 1998-11-03 2000-05-11 Basf Aktiengesellschaft Substituted 2-phenylbenzimidazoles, the production thereof and their use

Family Cites Families (181)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3914250A (en) 1974-08-01 1975-10-21 American Home Prod 1,4-Diazepino{8 6,5,4-jk{9 carbazoles
JPS608117B2 (en) 1977-02-08 1985-02-28 財団法人微生物化学研究会 New physiologically active substance esterastin and its production method
DE2928485A1 (en) 1979-07-14 1981-01-29 Bayer Ag USE OF UREA DERIVATIVES AS A MEDICINAL PRODUCT IN THE TREATMENT OF FATTY METABOLISM DISORDERS
US4476680A (en) 1979-08-14 1984-10-16 Sundstrand Corporation Pressure override control
ZA821577B (en) 1981-04-06 1983-03-30 Boots Co Plc Therapeutic agents
US4452813A (en) 1981-05-22 1984-06-05 Taiho Pharmaceutical Company Limited Sulfonate derivatives, process for preparing same and antilipemic compositions containing the derivative
CA1258454A (en) 1982-08-10 1989-08-15 Leo Alig Phenethanolamines
IT1159765B (en) 1982-09-28 1987-03-04 Zanussi A Spa Industrie MODULAR TYPE WASHING MACHINE
CA1247547A (en) 1983-06-22 1988-12-28 Paul Hadvary Leucine derivatives
IE61928B1 (en) 1988-11-29 1994-11-30 Boots Co Plc Treatment of obesity
US5391571A (en) 1989-11-15 1995-02-21 American Home Products Corporation Cholesterol ester hydrolase inhibitors
US5112820A (en) 1990-03-05 1992-05-12 Sterling Drug Inc. Anti-glaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-(1,2,3-de)-1,4-benzoxazines and method of use thereof
US5081122A (en) 1990-03-05 1992-01-14 Sterling Drug Inc. Antiglaucoma compositions containing 4-arylcarbonyl-1-(4-morpholinyl)-lower-alkyl)-1H-indoles and method of use thereof
US4973587A (en) 1990-03-08 1990-11-27 Sterling Drug Inc. 3-arylcarbonyl-1-aminoalkyl-1H-indole-containing antiglaucoma method
US5013837A (en) 1990-03-08 1991-05-07 Sterling Drug Inc. 3-Arylcarbonyl-1H-indole-containing compounds
US5321039A (en) 1990-04-13 1994-06-14 Societe Civile Bioprojet Method of inducing a histamine agonist action on H2 receptors
EP0503411B1 (en) * 1991-03-14 1995-11-29 BASF Aktiengesellschaft Substituted N-phenylpiperidines and medicaments thereof
DE4117904A1 (en) 1991-05-31 1992-12-03 Basf Ag SUBSTITUTED N-PHENYLPIPERIDINES
FR2692575B1 (en) 1992-06-23 1995-06-30 Sanofi Elf NOVEL PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
US6472178B1 (en) 1998-02-27 2002-10-29 Regeneron Pharmaceuticals, Inc. Nucleic acids encoding a modified ciliary neurotrophic factor and method of making thereof
US5349056A (en) 1992-10-09 1994-09-20 Regeneron Pharmaceuticals Modified ciliary neurotrophic factors
US5451677A (en) 1993-02-09 1995-09-19 Merck & Co., Inc. Substituted phenyl sulfonamides as selective β 3 agonists for the treatment of diabetes and obesity
US5292736A (en) 1993-02-26 1994-03-08 Sterling Winthrop Inc. Morpholinoalkylindenes as antiglaucoma agents
FR2714057B1 (en) 1993-12-17 1996-03-08 Sanofi Elf New derivatives of 3-pyrazolecarboxamide, process for their preparation and pharmaceutical compositions containing them.
US5705515A (en) 1994-04-26 1998-01-06 Merck & Co., Inc. Substituted sulfonamides as selective β-3 agonists for the treatment of diabetes and obesity
MX9702531A (en) * 1994-10-07 1997-06-28 Fujisawa Pharmaceutical Co Cyclic hexapeptides having antibiotic activity.
AU692977B2 (en) 1994-11-07 1998-06-18 Pfizer Inc. Certain substituted benzylamine derivatives; a new class of neuropeptide Y1 specific ligands
WO1996023517A1 (en) 1995-01-31 1996-08-08 Eli Lilly And Company Anti-obesity proteins
US5552523A (en) 1995-01-31 1996-09-03 Eli Lilly And Company Anti-obesity proteins
US5605886A (en) 1995-01-31 1997-02-25 Eli Lilly And Company Anti-obesity proteins
US5559208A (en) 1995-01-31 1996-09-24 Eli Lilly And Company Anti-obesity proteins
US5552524A (en) 1995-01-31 1996-09-03 Eli Lilly And Company Anti-obesity proteins
US5521283A (en) 1995-01-31 1996-05-28 Eli Lilly And Company Anti-obesity proteins
EP0836620A1 (en) 1995-01-31 1998-04-22 Eli Lilly And Company Anti-obesity proteins
US5554727A (en) 1995-01-31 1996-09-10 Eli Lilly And Company Anti-obesity proteins
US5552522A (en) 1995-01-31 1996-09-03 Eli Lilly And Company Anti-obesity proteins
US5532237A (en) 1995-02-15 1996-07-02 Merck Frosst Canada, Inc. Indole derivatives with affinity for the cannabinoid receptor
FR2732017B1 (en) 1995-03-21 2000-09-22 Inst Nat Sante Rech Med NOVEL IMIDAZOLE DERIVATIVES AND / OR HISTAMINE H3 RECEPTOR AGONISTS AND / OR AGONISTS, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATIONS
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
US20020006964A1 (en) 1995-05-16 2002-01-17 Young James W. Methods of using and compositions comprising (+) sibutramine optionally in combination with other pharmacologically active compounds
US5739106A (en) 1995-06-07 1998-04-14 Rink; Timothy J. Appetite regulating compositions
FR2741621B1 (en) 1995-11-23 1998-02-13 Sanofi Sa NOVEL PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
AU7692696A (en) 1995-12-01 1997-06-27 Novartis Ag Heteroaryl derivatives
WO1997020820A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
WO1997020823A2 (en) 1995-12-01 1997-06-12 Novartis Ag 2-amino quinazoline derivatives as npy receptor antagonists
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
US6017919A (en) 1996-02-06 2000-01-25 Japan Tobacco Inc. Compounds and pharmaceutical use thereof
EP0882038B1 (en) 1996-02-21 2002-12-18 Aventis Pharmaceuticals Inc. substituted n-methyl-n-(4-(piperidin-1-yl)-2-(aryl)butyl)benzamides useful for the treatment of allergic diseases
IT1288388B1 (en) 1996-11-19 1998-09-22 Angeletti P Ist Richerche Bio USE OF SUBSTANCES THAT ACTIVATE THE CNTF RECEPTOR (NEUROTROPHIC CHILI FACTOR) FOR THE PREPARATION OF DRUGS FOR THERAPY
WO1998027063A1 (en) 1996-12-16 1998-06-25 Banyu Pharmaceutical Co., Ltd. Aminopyrazole derivatives
DE69822449T2 (en) 1997-01-21 2005-01-27 Smithkline Beecham Corp. NEW CANNABINOID RECEPTOR MODULATORS
CN1246845A (en) 1997-02-04 2000-03-08 纳幕尔杜邦公司 Fungicidal carboxamides
SI0966436T1 (en) 1997-02-21 2003-04-30 Bayer Aktiengesellschaft Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
WO1998041519A1 (en) 1997-03-18 1998-09-24 Smithkline Beecham Corporation Novel cannabinoid receptor agonists
FR2761265B1 (en) 1997-03-28 1999-07-02 Sanofi Sa PHARMACEUTICAL COMPOSITION FOR THE ORAL ADMINISTRATION OF A DERIVATIVE OF N-PIPERIDINO-3-PYRAZOLECARBOXAMIDE, ITS SALTS AND THEIR SOLVATES
FR2761266B1 (en) 1997-03-28 1999-07-02 Sanofi Sa PHARMACEUTICAL COMPOSITION FORMED BY WET GRANULATION FOR THE ORAL ADMINISTRATION OF A DERIVATIVE OF N-PIPERIDINO-3- PYRAZOLECARBOXAMIDE, ITS SALTS AND THEIR SOLVATES
US6258837B1 (en) 1997-04-23 2001-07-10 Banyu Pharmaceutical Co., Ltd. Neuropeptide Y receptor antagonist
US6001836A (en) 1997-05-28 1999-12-14 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: cyanoguanidine derivatives
SE9702457D0 (en) 1997-06-26 1997-06-26 Pharmacia & Upjohn Ab screening
AU8127998A (en) 1997-07-11 1999-02-08 Japan Tobacco Inc. Quinoline compounds and medicinal uses thereof
CA2309121A1 (en) 1997-11-07 1999-05-20 Schering Corporation Phenyl-alkyl-imidazoles as h3 receptor antagonists
EP1068207A1 (en) 1998-04-02 2001-01-17 Neurogen Corporation AMINOALKYL SUBSTITUTED 9H-PYRIDINO 2,3-b]INDOLE AND 9H-PYRIMIDINO 4,5-b]INDOLE DERIVATIVES
HUP0102656A3 (en) 1998-04-29 2002-12-28 Ortho Mcneil Pharm Inc N-substituted aminotetralins as ligands for the neuropeptide y y5 receptor useful in the treatment of obesity and other disorders and medicaments containing them
US6329395B1 (en) 1998-06-08 2001-12-11 Schering Corporation Neuropeptide Y5 receptor antagonists
EP1085869A4 (en) 1998-06-11 2001-10-04 Merck & Co Inc Spiropiperidine derivatives as melanocortin receptor agonists
DE19837627A1 (en) 1998-08-19 2000-02-24 Bayer Ag New aminoacid esters of arylsulfonamides are useful for e.g. treating neurodegenerative diseases, pain, convulsions or bacterial or viral infections
HN1998000027A (en) 1998-08-19 1999-06-02 Bayer Ip Gmbh Arylsulphonamides and analogues
US6358951B1 (en) 1998-08-21 2002-03-19 Pfizer Inc. Growth hormone secretagogues
US6337332B1 (en) 1998-09-17 2002-01-08 Pfizer Inc. Neuropeptide Y receptor antagonists
PT1121111E (en) 1998-10-15 2010-05-17 Imp Innovations Ltd Compounds for the treatment of weight loss
ATE314371T1 (en) 1998-11-10 2006-01-15 Merck & Co Inc SPIRO-INDOLE AS Y5 RECEPTOR ANTAGONISTS
US6344481B1 (en) 1999-03-01 2002-02-05 Pfizer Inc. Thyromimetic antiobesity agents
PL351963A1 (en) 1999-03-19 2003-07-14 Knoll Gmbh Method of treating eating disorders
US6340683B1 (en) 1999-04-22 2002-01-22 Synaptic Pharmaceutical Corporation Selective NPY (Y5) antagonists (triazines)
DE60034783T2 (en) 1999-04-22 2008-01-31 H. Lundbeck A/S, Valby SELECTIVE NPY (Y5) ANTAGONISTS
MXPA01011321A (en) 1999-05-05 2003-08-01 Johnson & Johnson 3a,4,5,9b-TETRAHYDRO-1H-BENZ[e]INDOL-2-YL AMINE-DERIVED NEUROPEPTIDE Y RECEPTORS LIGANDS USEFUL IN THE TREATMENT OF OBESITY AND OTHER DISORDERS.
DE60023128T2 (en) 1999-05-12 2006-07-06 Ortho-Mcneil Pharmaceutical, Inc. PYRAZOL CARBOXAMIDE FOR THE TREATMENT OF FATIBILITY AND OTHER DISORDERS
JP2003503486A (en) 1999-06-30 2003-01-28 シナプティック・ファーマスーティカル・コーポレーション Selective NPY (Y5) antagonist
AU6000900A (en) 1999-07-23 2001-02-13 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
AR030676A1 (en) 1999-07-28 2003-09-03 Ortho Mcneil Pharm Inc DERIVATIVES OF AMINAS AND AMIDAS AS LINKS TO THE NEUROPEPTIDE RECEIVER AND Y5 USEFUL IN THE TREATMENT OF OBESITY AND OTHER DISORDERS, USE OF THE SAME FOR THE DEVELOPMENT OF PHARMACEUTICAL MEDICINES AND COMPOSITIONS THAT UNDERSTAND THEM
TWI279402B (en) 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
OA12049A (en) 1999-09-30 2006-05-02 Neurogen Corp Amino substituted pyrazoloÄ1,5,-aÜ-1,5-pyrimidinesand pyrazoloÄ1,5,-aÜ-1,3,5-triazines.
IL148905A0 (en) 1999-09-30 2002-09-12 Neurogen Corp Pfizer Inc Certain alkylene diamine-substituted pyrazolo{1,5,-a}-1,5-pyrimidines and pyrazolo{1,5,-a}-1,3,5-triazines
DE60026155T2 (en) 1999-09-30 2006-08-10 Neurogen Corp., Branford SOME ALKYLENDIAMINE-SUBSTITUTED HETEROCYCLES
DE19949319A1 (en) 1999-10-13 2001-06-13 Ruetgers Vft Ag Process for the preparation of aryl alkyl ethers
EA005671B1 (en) 1999-10-13 2005-04-28 Пфайзер Продактс Инк. Biaryl ether derivatives useful as monoamine reuptake inhibitors
US6239395B1 (en) 1999-10-14 2001-05-29 General Electric Company Auxiliary position switch assembly for a circuit breaker
NZ519272A (en) 1999-12-16 2004-02-27 Schering Corp Substituted imidazole neuropeptide Y Y5 receptor antagonists
AU2001228325A1 (en) 2000-02-01 2001-08-14 Novo-Nordisk A/S Use of compounds for the regulation of food intake
CA2399791A1 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
JP2001226269A (en) 2000-02-18 2001-08-21 Takeda Chem Ind Ltd Melanin-concentrating hormone antagonist
GB0004003D0 (en) 2000-02-22 2000-04-12 Knoll Ag Therapeutic agents
DE60109756T2 (en) 2000-02-22 2005-08-25 Banyu Pharmaceutical Co., Ltd. IMIDAZOLINE CONNECTIONS
US6531478B2 (en) 2000-02-24 2003-03-11 Cheryl P. Kordik Amino pyrazole derivatives useful for the treatment of obesity and other disorders
FR2805818B1 (en) 2000-03-03 2002-04-26 Aventis Pharma Sa AZETIDINE DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2805810B1 (en) 2000-03-03 2002-04-26 Aventis Pharma Sa PHARMACEUTICAL COMPOSITIONS CONTAINING 3- AMINO-AZETIDINE DERIVATIVES, THE NEW DERIVATIVES AND THEIR PREPARATION
FR2805817B1 (en) 2000-03-03 2002-04-26 Aventis Pharma Sa PHARMACEUTICAL COMPOSITIONS CONTAINING AZETIDINE DERIVATIVES, NOVEL AZETIDINE DERIVATIVES AND THEIR PREPARATION
EP1132389A1 (en) 2000-03-06 2001-09-12 Vernalis Research Limited New aza-indolyl derivatives for the treatment of obesity
ES2234840T3 (en) 2000-03-14 2005-07-01 Actelion Pharmaceuticals Ltd. DERIVATIVES OF 1,2,3,4- TETRAHYDROISOQUINOLINE.
AU4928101A (en) 2000-03-23 2001-10-03 Merck & Co Inc Spiropiperidine derivatives as melanocortin receptor agonists
AU4929601A (en) 2000-03-23 2001-10-03 Merck & Co Inc Substituted piperidines as melanocortin receptor agonists
US6600015B2 (en) 2000-04-04 2003-07-29 Hoffmann-La Roche Inc. Selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity
EP1142886A1 (en) 2000-04-07 2001-10-10 Aventis Pharma Deutschland GmbH Percyquinnin, a process for its production and its use as a pharmaceutical
DK1285651T3 (en) 2000-04-28 2010-12-13 Takeda Pharmaceutical Melanin-concentrating hormone antagonists
GB0010757D0 (en) 2000-05-05 2000-06-28 Astrazeneca Ab Chemical compounds
GB0011013D0 (en) 2000-05-09 2000-06-28 Astrazeneca Ab Chemical compounds
US6444675B2 (en) 2000-05-10 2002-09-03 Bristol-Myers Squibb Company 4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists
AU2001263021A1 (en) 2000-05-10 2001-11-20 Bristol-Myers Squibb Company Alkylamine derivatives of dihydropyridine npy antagonists
US6432960B2 (en) 2000-05-10 2002-08-13 Bristol-Myers Squibb Company Squarate derivatives of dihydropyridine NPY antagonists
EP1280777B1 (en) 2000-05-11 2005-11-23 Bristol-Myers Squibb Company Tetrahydroisoquinoline analogs useful as growth hormone secretagogues
EP1283199A4 (en) 2000-05-16 2003-12-17 Takeda Chemical Industries Ltd Melanin-concentrating hormone antagonist
AUPQ761100A0 (en) 2000-05-18 2000-06-08 Australian Rural Group Limited Lipophilic medicament
US6391881B2 (en) 2000-05-19 2002-05-21 Bristol-Myers Squibb Company Thiourea derivatives of dihydropyridine NPY antagonists
SE0001899D0 (en) 2000-05-22 2000-05-22 Pharmacia & Upjohn Ab New compounds
AU2001264977B2 (en) 2000-05-30 2005-04-14 Merck & Co., Inc. Melanocortin receptor agonists
PT1294714E (en) 2000-06-15 2007-11-06 Schering Corp Thrombin receptor antagonists
US6677354B2 (en) 2000-06-16 2004-01-13 Smithkline Beecham P.L.C. Piperdines for use as orexin receptor antagonists
WO2002006245A1 (en) 2000-07-05 2002-01-24 Synaptic Pharmarceutical Corporation Selective melanin concentrating hormone-1 (mch1) receptor antagonists and uses thereof
WO2002004433A2 (en) 2000-07-06 2002-01-17 Neurogen Corporation Melanin concentrating hormone receptor ligands
GB0019357D0 (en) 2000-08-07 2000-09-27 Melacure Therapeutics Ab Novel phenyl guanidines
US20020187938A1 (en) 2000-07-24 2002-12-12 Romano Deghenghi Ghrelin antagonists
WO2002010169A1 (en) 2000-07-31 2002-02-07 F. Hoffmann-La Roche Ag Piperazine derivatives
US6768024B1 (en) 2000-08-04 2004-07-27 Lion Bioscience Ag Triamine derivative melanocortin receptor ligands and methods of using same
GB0019359D0 (en) 2000-08-07 2000-09-27 Melacure Therapeutics Ab Novel guanidines
AU2001288294A1 (en) 2000-08-21 2002-03-04 Merck And Co., Inc. Anti-hypercholesterolemic drug combination
JP2004506685A (en) 2000-08-21 2004-03-04 グリアテツク・インコーポレイテツド Use of histamine H3 receptor inverse agonists for controlling appetite and treating obesity
CA2419310A1 (en) 2000-08-23 2002-02-28 Merck & Co., Inc. Substituted piperidines as melanocortin receptor agonists
US6900226B2 (en) 2000-09-06 2005-05-31 Hoffman-La Roche Inc. Neuropeptide Y antagonists
AU2001294547A1 (en) 2000-09-14 2002-03-26 Schering Corporation Substituted urea neuropeptide y y5 receptor antagonists
BR0114630A (en) 2000-10-13 2003-07-01 Lilly Co Eli Growth Hormone Secretagogues
DE10050995A1 (en) 2000-10-14 2002-04-18 Boehringer Ingelheim Pharma New benzylic acid azabicyclooctane ester quaternary salts useful as anticholinergic agents, especially in treatment of asthma and chronic obstructive pulmonary disease
AR038762A1 (en) 2000-10-16 2005-01-26 Hoffmann La Roche DERIVATIVES OF INDOLINA, A PROCESS FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION, PROCESS FOR THE PREPARATION OF SUCH COMPOSITION AND THE USE OF SUCH DERIVATIVES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT
WO2002036596A2 (en) 2000-11-03 2002-05-10 Wyeth CYCLOALKYL[b][1,4]DIAZEPINO[6,7,1-hi]INDOLES AND DERIVATIVES
AU1529402A (en) 2000-11-20 2002-05-27 Biovitrum Ab Piperazinylpyrazines compounds as antagonists of serotonin 5-ht2 receptor
CA2448729A1 (en) 2000-11-20 2002-05-23 Biovitrum Ab Piperazinyl and piperidyl substituted heterocyclic compounds
EP1347982B1 (en) 2000-12-12 2005-11-16 Neurogen Corporation Spiro isobenzofuran-1,4'-piperidin]-3-ones and 3h-spiroisobenzofuran-1,4'-piperidines
GB0030710D0 (en) 2000-12-15 2001-01-31 Hoffmann La Roche Piperazine derivatives
EP1343503B1 (en) 2000-12-21 2008-11-12 Schering Corporation Heteroaryl urea neuropeptide y y5 receptor antagonists
CA2431953A1 (en) 2000-12-22 2002-07-04 Schering Corporation Piperidine mch antagonists and their use in the treatment of obesity
WO2002051844A1 (en) 2000-12-27 2002-07-04 F. Hoffmann-La Roche Ag Indole derivatives and their use as 5-ht2b and 5-ht2c receptor ligands
WO2002051232A2 (en) 2000-12-27 2002-07-04 Actelion Pharmaceuticals Ltd. Novel benzazepines and related heterocyclic derivatives
US7157463B2 (en) 2001-01-23 2007-01-02 Eli Lilly And Company Substituted piperidines/piperazines as melanocortin receptor agonists
JP2004523530A (en) 2001-01-23 2004-08-05 イーライ・リリー・アンド・カンパニー Piperazine and piperidine derivatives as melanocortin receptor agonists
US7169777B2 (en) 2001-01-23 2007-01-30 Eli Lilly And Company Melanocortin receptor agonists
CA2437492A1 (en) 2001-02-02 2002-08-15 Yoshihiro Banno Fused heterocyclic compounds
EP1372653B1 (en) 2001-02-28 2006-10-04 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
JP4316238B2 (en) 2001-02-28 2009-08-19 メルク エンド カムパニー インコーポレーテッド Acylated piperidine derivatives as melanocortin-4 receptor agonists
HUP0303376A3 (en) 2001-02-28 2007-08-28 Merck & Co Inc Acylated piperidine derivatives as melanocortin-4 receptor agonists, and pharmaceutical compositions containing them and use thereof
CN100537527C (en) 2001-03-21 2009-09-09 法马科皮亚公司 Aryl and biaryl compounds having MCH modulatory activity
US6900329B2 (en) 2001-03-21 2005-05-31 Schering Corporation MCH antagonists and their use in the treatment of obesity
CA2422708C (en) 2001-03-22 2010-10-26 Solvay Pharmaceuticals B.V. 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
EP1379493A2 (en) 2001-03-23 2004-01-14 Eli Lilly and Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
AU782148B2 (en) 2001-03-29 2005-07-07 Molecular Design International, Inc. Beta3-adrenoreceptor agonists, agonist compositions and methods of making and using the same
WO2002083134A1 (en) 2001-04-12 2002-10-24 Pharmacopeia, Inc. Aryl and biaryl piperidines used as mch antagonists
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
FR2824825B1 (en) 2001-05-15 2005-05-06 Servier Lab NOVEL ALPHA-AMINOACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
EP1395564B1 (en) 2001-05-21 2008-02-27 F. Hoffmann-La Roche Ag Quinoline derivatives as ligands for the neuropeptide y receptor
IL158941A0 (en) 2001-05-22 2004-05-12 Neurogen Corp Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues
WO2002099388A2 (en) 2001-06-07 2002-12-12 Merck & Co., Inc. Benzodiazepine bradykinin antagonists
CA2450475A1 (en) 2001-06-20 2003-01-03 Linda Brockunier Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2004535433A (en) 2001-06-20 2004-11-25 メルク エンド カムパニー インコーポレーテッド Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
ES2291477T3 (en) 2001-06-27 2008-03-01 Smithkline Beecham Corporation FLUOROPIRROLIDINS AS INHIBITORS OF DIPEPTIDIL PEPTIDASA.
JPWO2003002539A1 (en) 2001-06-27 2004-10-14 宇部興産株式会社 Dibenzocycloheptene compound
CN1723196A (en) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
WO2003002530A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
ATE388951T1 (en) 2001-07-03 2008-03-15 Novo Nordisk As DPP-IV INHIBITING PURINE DERIVATIVES FOR THE TREATMENT OF DIABETES
HUP0401880A2 (en) 2001-07-05 2005-01-28 Synaptic Pharmaceutical Corporation Substituted anilinic piperidines as mch selective antagonists, pharmaceutical compositions containing them and their use
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
ITMI20011483A1 (en) 2001-07-11 2003-01-11 Res & Innovation Soc Coop A R USE OF COMPOUNDS AS FUNCTIONAL ANTAGONISTS TO CENTRAL DEICANNABINOID RECEPTORS
WO2003007949A1 (en) 2001-07-18 2003-01-30 Merck & Co., Inc. Bridged piperidine derivatives as melanocortin receptor agonists
WO2003007887A2 (en) 2001-07-20 2003-01-30 Merck & Co., Inc. Substituted imidazoles as cannabinoid receptor modulators
US6977264B2 (en) 2001-07-25 2005-12-20 Amgen Inc. Substituted piperidines and methods of use
US6915444B2 (en) 2001-09-12 2005-07-05 Rockwell Automation Technologies, Inc. Network independent safety protocol for industrial controller using data manipulation techniques
WO2003062234A1 (en) * 2002-01-23 2003-07-31 Yamanouchi Pharmaceutical Co., Ltd. Quinoxaline compounds
EP1556046A1 (en) * 2002-10-23 2005-07-27 Janssen Pharmaceutica N.V. Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators
US20040192728A1 (en) 2003-02-03 2004-09-30 Ellen Codd Quinoline-derived amide modulators of vanilloid VR1 receptor
UY28506A1 (en) * 2003-09-12 2005-04-29 Basf Ag 6-HALOGEN- (1,2,4) TRIAZOL (1,5-A) PYRIMIDINS TO COMBAT ANIMAL PESTS.
AU2004274309B2 (en) * 2003-09-22 2010-04-08 Msd K.K. Novel piperidine derivative

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3951982A (en) * 1974-11-21 1976-04-20 Parke, Davis & Company Trialkylsilyl esters of 6(substituted amino)phenyl-1,-dihydro-2-oxonicotinic acid, methods for their production and conversion to the corresponding acid chlorides
WO2000026192A1 (en) * 1998-11-03 2000-05-11 Basf Aktiengesellschaft Substituted 2-phenylbenzimidazoles, the production thereof and their use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; GOEL, OM P.: "Trialkylsilyl esters of 6-(substituted amino)phenyl-1, dihydro-2-oxonicotinic acid and conversion to the corresponding acid chlorides", XP002520492, retrieved from STN Database accession no. 1976:543094 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; LUBISCH, WILFRIED ET AL: "Preparation of 2-phenylbenzimidazoles as poly(ADP-ribose) polymerase inhibitors.", XP002520491, retrieved from STN Database accession no. 2000:314677 *

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